The present invention is concerned with compounds, compositions and methods useful for treating symptomologies in human beings which are affected by .alpha..sub.2 blockade. In particular, compounds wherein benzodioxane is linked through 0 to 3 methylene groups to an imidazoline nucleus are thus useful.
Large numbers of compounds are known which affect various physiological systems related to synaptic control. The class most closely related to the compounds of the present invention is that disclosed in U.S. Pat. No. 2,979,511, issued Apr. 11, 1961 to Krapcho, et al. This patent purports to disclose, generically, some of the compounds of the present invention, specifically those wherein n is equal to 0 or 1, the R groups are hydrogen or lower alkyl, and R.sup.1 is hydrogen. Also, specifically claimed in the Krapcho patent are 2-(1,4-benzodioxan-2-yl)-imidazoline, and its hydrochloride. These compounds are disclosed as peripherally acting vasolidators. The methods of preparation given therein, do not, in our hands, yield the imidazoline ring, but rather the open chain counterparts.
The present invention concerns a suite of imidazoline compounds, which are attached to benzodioxane moiety through methylene chains varying from 0 to 3 methylene units, and which optionally carry aromatic as well as alkyl substituents.
These compounds have .alpha..sub.2 blocking activity.